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181. 发明授权

US5411947A Method of converting a drug to an orally available form by covalently bonding a lipid to the drug 失效
标题翻译：通过将脂质共价键合到药物来将药物转化成口服形式的方法
公开(公告)号：US5411947A
公开(公告)日：1995-05-02
申请号：US991166
申请日：1992-12-16
申请人： Karl Y. Hostetler , Raj Kumar
发明人： Karl Y. Hostetler , Raj Kumar
IPC分类号： A61K47/48 , A61K9/127 , A61K31/337 , A61P35/00 , C07F9/38 , C07F9/40 , C07F9/655 , C07H15/04 , C07H19/06 , C07H19/16 , A01N43/04 , A01N37/18 , A61K31/43 , A61K38/00
CPC分类号： C07H15/04 , A61K47/48023 , A61K47/48038 , A61K47/48053 , A61K47/48084 , A61K9/127 , B82Y5/00 , C07F9/3891 , C07F9/4006 , C07F9/4065 , C07F9/65512 , C07H19/06 , C07H19/16 , Y10S514/885
摘要： The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.
摘要翻译：通过将具有合适的官能团的药物转化为1-O-烷基 - ，1-O-酰基 - ，1-S-酰基和1-S-烷基-sn-甘油基-3，可促进许多类药物的口服递送磷酸酯衍生物。该方法赋予了在非衍生化状态下不经口服生物利用的药物通过消化道吸收的能力，并提高吸收不良或快速消除的药物的有效性。该方法提供具有不同生理活性的药物化合物的口服生物可利用的脂前药，包括抗癌和抗病毒剂，抗炎药，抗高血压药和抗生素。脂质前药的效力与相应的非衍生化药物的效力相当。

182. 发明授权

US5409705A Phosphobetaine and detergent and cosmetic containing the same 失效
标题翻译：磷酸甜菜碱和洗涤剂和化妆品含有相同的含量
公开(公告)号：US5409705A
公开(公告)日：1995-04-25
申请号：US796337
申请日：1991-11-22
申请人： Katsumi Kita , Mitsuru Uno , Hiroshi Kamitani , Yoshiaki Fujikura , Nobutaka Horinishi , Tomohito Kitsuki , Kazuyasu Imai , Yasushi Kajihara
发明人： Katsumi Kita , Mitsuru Uno , Hiroshi Kamitani , Yoshiaki Fujikura , Nobutaka Horinishi , Tomohito Kitsuki , Kazuyasu Imai , Yasushi Kajihara
IPC分类号： C07F9/09 , C07F9/655 , C07H11/04 , C07H15/04 , C08B31/06 , C11D1/88 , C11D3/22 , C11D3/36 , C07C69/76 , A61K7/06 , C07H15/00
CPC分类号： C11D3/364 , A61K8/55 , A61Q19/00 , C07F9/091 , C07F9/65515 , C07H11/04 , C07H15/04 , C08B31/066 , C11D1/886 , C11D3/228 , A61Q19/10 , A61Q5/00 , A61Q5/006 , A61Q5/02
摘要： A novel phosphobetaine is disclosed. This compound is very excellence in that it exerts a conditioning effect of imparting a good feel to the skin or hair, is excellent in humidifying properties, is available at a low price, and thus it is highly usable in detergents, cosmetics, a bathing preparation and the like. A detergent composition, a cosmetic, and a bathing preparation each containing the phosphobetaine are also disclosed.
摘要翻译：公开了一种新的磷酸甜菜碱。该化合物非常优异地发挥赋予皮肤或毛发良好感觉的调理效果，加湿性优异，可以低价位获得，因此其可用于洗涤剂，化妆品，洗浴用品等等。还公开了含有磷酸甜菜碱的洗涤剂组合物，化妆品和洗浴剂。

183. 发明授权

US5393877A Linkers for the synthesis of multiple oligonucleotides in seriatim from a single support attachment 失效
标题翻译：用于从单个支持附件合成多个寡核苷酸的连接体
公开(公告)号：US5393877A
公开(公告)日：1995-02-28
申请号：US41599
申请日：1993-04-05
申请人： Michael J. McLean , David Holland , Andrew J. Garman , Robert C. Sheppard
发明人： Michael J. McLean , David Holland , Andrew J. Garman , Robert C. Sheppard
IPC分类号： C12N15/09 , C07F9/655 , C07H21/00 , C07H21/04
CPC分类号： C07F9/65515 , C07H21/00
摘要： A method for the synthesis of a plurality of oligonucleotides comprising the steps of(i) forming a first oligonucleotide on a first cleavable link attached to a solid support;(ii) attaching to the first oligonucleotide a cleavable linker moiety;(iii) forming a second oligonucleotide on the cleavable linker moiety; and(iv) cleaving the first cleavable link and the cleavable linker moiety to give a plurality of oligonucleotides; wherein the cleavable linker moiety is of the Formula (1): ##STR1## in which A.sup.1, A.sup.2 and E are as defined herein, and novel compounds which may be used in the operation of the method.
摘要翻译：一种用于合成多种寡核苷酸的方法，包括以下步骤：（i）在连接到固体支持物上的第一可切割链节上形成第一寡核苷酸; （ii）将第一寡核苷酸连接到可切割的接头部分上; （iii）在可切割接头部分上形成第二寡核苷酸; 和（iv）切割第一可切割连接和可切割连接部分以产生多个寡核苷酸; 其中所述可切割接头部分具有式（1）：其中A1，A2和E如本文所定义的式（1）和可用于该方法操作的新化合物。

184. 发明授权

US5393729A 3-aryl-pyrone derivatives 失效
标题翻译： 3-芳基 - 吡喃酮衍生物
公开(公告)号：US5393729A
公开(公告)日：1995-02-28
申请号：US116790
申请日：1993-09-03
申请人： Reiner Fischer , Andreas Krebs , Folker Lieb , Michael Ruther , Jorg Stetter , Christoph Erdelen , Ulrike Wachendorff-Neumann , Klaus Lurssen , Hans-Joachim Santel , Robert R. Schmidt
发明人： Reiner Fischer , Andreas Krebs , Folker Lieb , Michael Ruther , Jorg Stetter , Christoph Erdelen , Ulrike Wachendorff-Neumann , Klaus Lurssen , Hans-Joachim Santel , Robert R. Schmidt
IPC分类号： A01N43/16 , A01N43/40 , A01N43/90 , A01N47/06 , A01N57/24 , A61K31/35 , A61K31/351 , A61K31/365 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P33/00 , C07D309/36 , C07D309/38 , C07D311/74 , C07D311/94 , C07D405/04 , C07D407/04 , C07D407/12 , C07D409/04 , C07D493/04 , C07D495/04 , C07F9/655
CPC分类号： C07D405/04 , A01N43/16 , A01N43/40 , A01N43/90 , A01N47/06 , A01N57/24 , C07D309/38 , C07D311/74 , C07D311/94 , C07D407/04 , C07D409/04 , C07D493/04 , C07D495/04 , C07F9/6552
摘要： The invention relates to 3-aryl-pyrone derivatives of the general formula (I) ##STR1## in which the substituents are as defined in the specification. The compounds are useful as pesticides, herbicides and fungicides.
摘要翻译：本发明涉及通式（I）的3-芳基 - 吡喃酮衍生物，其中取代基如说明书中所定义。这些化合物可用作农药，除草剂和杀真菌剂。

185. 发明授权

US5369127A 1,3-benzodioxole and 1,2-dialkoxybenzene derivatives as ocular hypotensive agents 失效
标题翻译： 1,3-苯并间二氧杂环戊烯和1,2-二烷氧基苯衍生物作为低血压剂
公开(公告)号：US5369127A
公开(公告)日：1994-11-29
申请号：US51104
申请日：1993-04-21
申请人： Robert M. Burk , David F. Woodward
发明人： Robert M. Burk , David F. Woodward
IPC分类号： A61K31/075 , A61K31/135 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/27 , A61K31/335 , A61K31/34 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/66 , A61P27/02 , C07C43/23 , C07C59/64 , C07C69/734 , C07D307/36 , C07D317/54 , C07D317/60 , C07D319/08 , C07D333/16 , C07F7/18 , C07F9/655
CPC分类号： C07D317/60 , C07C43/23 , C07C59/64 , C07C69/734 , C07D317/54
摘要： Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is O and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5, R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CHOR.sub.9 O, --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.9 is divalent alkyl radical of 2-5 carbons, R.sub.10 is an alkyl OR cycloalkyl containing 1 to 5 carbons;R.sub.2 is H, COR.sub.7, R.sub.7, CO--OR.sub.7, CO--NR.sub.5, R.sub.7, PO(OH)OR.sub.7, PO(OR.sub.7).sub.2, POR.sub.7 OH, or POR.sub.7 (OR.sub.7);R.sub.3 is lower alkyl, phenyl, lower alkyl or halogen substituted phenyl, phenyl substituted lower alkyl, or heteroaryl substituted lower alkyl, are capable of lowering introaocular pressure in the eye of a mammal.
摘要翻译：其中W为（CH 2）n，其中n为1或2，或n为O且W为连接至每个氧的低级烷基的式IMAMA的化合物; m是1和8之间的整数; R1是COOH或其药学上可接受的盐，COOR4，CONR5R6，CONR5SO2R7，CH2OH，CH2OR7，CH2O-COR7，CH2O-CONR5，R7，CH2OCOOR7，CH2NH2，CH2NR5R6，CH2NR5COR7，CHO，CH（OR8）2，CHOR9O，，CR10（OR8）2或CR10OR9O，其中R4是1〜10个碳原子的烷基或5〜10个碳原子的环烷基，或R4是苯基或低级烷基苯基，R5和R6独立地是氢，烷基 1〜10个碳原子的环烷基或5〜10个碳的环烷基，或苯基或低级烷基苯基，R7为1〜10个碳原子的烷基，苯基或低级烷基苯基，R8为低级烷基，R9为2- 5个碳原子，R10是含1至5个碳原子的烷基OR环烷基; R2是H，COR7，R7，CO-OR7，CO-NR5，R7，PO（OH）OR7，PO（OR7）2，POR7OH或POR7（OR7） R3是低级烷基，苯基，低级烷基或卤素取代的苯基，苯基取代的低级烷基或杂芳基取代的低级烷基，能够降低哺乳动物眼睛的眼内压。

186. 发明授权

US5367066A Oligonucleotides with selectably cleavable and/or abasic sites 失效
标题翻译：具有可选择性切割和/或非碱性位点的寡核苷酸
公开(公告)号：US5367066A
公开(公告)日：1994-11-22
申请号：US736445
申请日：1991-07-24
申请人： Michael S. Urdea , Thomas Horn
发明人： Michael S. Urdea , Thomas Horn
IPC分类号： C07F9/10 , C07F9/24 , C07F9/655 , C07H15/18 , C07H19/06 , C07H19/10 , C07H21/00 , C07H23/00 , C12Q1/68 , C07H21/04
CPC分类号： C07F9/10 , C07F9/2429 , C07F9/65515 , C07H15/18 , C07H19/06 , C07H19/10 , C07H21/00 , C07H23/00 , C12Q1/6813 , C12Q1/6816 , C12Q1/6823 , C12Q1/6827 , C12Q1/683
摘要： A modified polynucleotide containing at least one cleavable or abasic site as shown below. ##STR1## DNA.sub.1 is a first segment of DNA; DNA.sub.2 is a second segment of DNA; and R.sub.m is C.sub.1 to C.sub.16 alkylene or an oxytheylene oligomer --(CH.sub.2 CH.sub.2 O).sub.z -- where z is an interger in the range of 1 to 16 inclusive, and R.sub.n is selected from the group consisting of ##STR2## Such polynucleotides are useful in solid phase hybridizations because they permit the release of a label from the solid support after the hybridization reaction.
摘要翻译：含有如下所示的至少一个可切割或非碱性位点的修饰的多核苷酸。 DNA1是DNA的第一段; DNA2是DNA的第二段; 且R m为C 1至C 16亚烷基或氧亚乙基低聚物 - （CH 2 CH 2 O）z - ，其中z为1至16的整数，其中R n选自图像>图像> CH3OCH2CH2OCH2。这样的多核苷酸可用于固相杂交，因为它们允许在杂交反应后从固体支持物释放标记物。

187. 发明授权

US5364564A Phosphatidyl chromanol derivative, the production method thereof, antioxidant and emulsifier 失效
标题翻译：磷脂酰基色胺醇衍生物，其制备方法，抗氧化剂和乳化剂
公开(公告)号：US5364564A
公开(公告)日：1994-11-15
申请号：US190479
申请日：1994-02-02
申请人： Takuro Koga
发明人： Takuro Koga
IPC分类号： B01F17/14 , A23L3/3544 , C07F9/10 , C07F9/655 , C09K15/32 , C07F9/12
CPC分类号： A23L3/3544 , C07F9/65522
摘要： The present invention relates to a phosphatidyl chromanol derivative having the formula: ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom, or a saturated or unsaturated fatty acid residue of 2-24 carbon numbers, n is an integer of 1-5 and X is a monovalent cation; a process for synthesizing the phosphatidyl chromanol derivative of the formula (3) which comprises reacting a phospholipid with a chroman derivative of the formula: ##STR2## wherein n is an integer of 1-5 using a phospholipase D and an antioxidant/emulsifier containing the compound of the formula (3).
摘要翻译：本发明涉及具有下式的磷脂酰基色胺醇衍生物：其中R1和R2表示氢原子，或2-24个碳数的饱和或不饱和脂肪酸残基，n为1- 5和X是一价阳离子; 一种用于合成式（3）的磷脂酰基苯并二氢吡喃衍生物的方法，其包括使磷脂与下式的苯并二氢吡喃衍生物反应：其中n是1-5的整数，使用磷脂酶D和抗氧化剂/ 含有式（3）化合物的乳化剂。

188. 发明授权

US5360817A Derivatives and analogues of 2-deoxy-2,3-didehydro-N-acetyl neuraminic acid and their use as antiviral agents 失效
标题翻译： 2-脱氧-2,3-二脱氢-N-乙酰神经氨酸的衍生物和类似物及其作为抗病毒剂的用途
公开(公告)号：US5360817A
公开(公告)日：1994-11-01
申请号：US946327
申请日：1992-11-10
申请人： Laurence M. von Izstein , Wen-Yang Wu , Tho V. Phan , Basil Danylec , Betty Jin
发明人： Laurence M. von Izstein , Wen-Yang Wu , Tho V. Phan , Basil Danylec , Betty Jin
IPC分类号： C07D309/30 , A61K31/00 , A61K31/196 , A61K31/34 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/41 , A61K31/435 , A61K31/44 , A61K31/505 , A61K31/7012 , A61P31/00 , A61P31/12 , A61P31/14 , C07C47/225 , C07C47/42 , C07C225/20 , C07C233/52 , C07C309/25 , C07C317/12 , C07C321/22 , C07D20060101 , C07D211/70 , C07D211/72 , C07D211/74 , C07D211/78 , C07D211/84 , C07D239/26 , C07D257/02 , C07D257/04 , C07D309/20 , C07D309/22 , C07D309/26 , C07D309/28 , C07D335/02 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D498/04 , C07F9/655 , C07H7/033
CPC分类号： C07D309/30 , C07D309/28
摘要： Derivatives and analogues of 2-deoxy-2,3-didehydro-N-acetyl neuraminic acid, pharmaceutical formulations thereof, methods for their preparation .and their use in the treatment of viral infections, in particular influenza, are described.
摘要翻译： PCT No.PCT / AU91 / 00161 Sec。 371日期：1992年11月10日 102（e）日期：1992年11月10日PCT 1991年4月24日PCT PCT。 WO91 / 16320 PCT公开号日期：1991年10月31日。2-脱氧-2,3-二脱氢-N-乙酰神经氨酸的衍生物和类似物，其药物制剂，其制备方法及其在治疗病毒感染中的用途，特别是流感，被描述。

189. 发明授权

US5356966A 3-(carboxymethoxyphenyl)benzofuran-2-one stabilizers 失效
公开(公告)号：US5356966A
公开(公告)日：1994-10-18
申请号：US64193
申请日：1993-05-17
申请人： Peter Nesvadba
发明人： Peter Nesvadba
IPC分类号： C07D307/80 , C07D307/83 , C07F9/655 , C08K5/15 , C08K5/1535 , C08K5/20 , C08K5/5373 , C09K3/00 , C09K15/04
CPC分类号： C07D307/83 , C07F9/65517 , C08K5/1535 , C08K5/20 , C08K5/5373
摘要： Compounds of the formula (1), ##STR1## in which R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, C.sub.1 -C.sub.25 alkyl, C.sub.7 -C.sub.9 phenylalkyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted phenyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.8 cycloalkyl; C.sub.1 -C.sub.18 alkoxy, hydroxyl, C.sub.1 -C.sub.25 alkanoyloxy, C.sub.3 -C.sub.25 alkenoyloxy, C.sub.3 -C.sub.25 alkanoyloxy which is interrupted by oxygen, sulfur or >N--R.sub.13 ; C.sub.6 -C.sub.9 cycloalkylcarbonyloxy, benzoyloxy or C.sub.1 -C.sub.12 alkyl-substituted benzoyloxy, in which R.sub.13 is hydrogen or C.sub.1 -C.sub.18 alkyl, or furthermore the radicals R.sub.2 and R.sub.3 or the radicals R.sub.4 and R.sub.5 together with the carbon atoms to which they are bonded form a phenyl ring, R.sub.4 is additionally (CH.sub.2).sub.n --COR.sub.14, in which n is 0, 1 or 2, R.sub.14 is hydroxyl, ##EQU1## C.sub.1 -C.sub.18 alkoxy or ##STR2## R.sub.15 and R.sub.16, independently of one another, are hydrogen or C.sub.1 -C.sub.18 alkyl, M is an r-valent metal cation and r is 1, 2 or 3, R.sub.7, R.sub.8, R.sub.9 and R.sub.10, independently of one another, are hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, with the proviso that at least one of the radicals R.sub.7, R.sub.8, R.sub.9 and R.sub.10 is hydrogen, R.sub.11 and R.sub.12, independently of one another, are hydrogen, C.sub.1 -C.sub.4 alkyl or phenyl, and, in the case where R.sub.3, R.sub.5, R.sub.6, R.sub.7 and R.sub.10 are hydrogen, R.sub.4 is additionally a radical of the formula (2), ##STR3## in which R.sub.2, R.sub.8, R.sub.9, R.sub.11 and R.sub.12 are as defined above and R.sub.1 is as defined below for m=1 and R.sub.17 and R.sub.18, independently of one another, are hydrogen, C.sub.1 -C.sub.12 alkyl or phenyl, or R.sub.17 and R.sub.18 together with the carbon atom to which they are bonded form a C.sub.5 -C.sub.7 cycloalkylidene ring which is unsubstituted or substituted by 1 to 3 C.sub.1 -C.sub.4 alkyl, m is an integer from the range of 1 to 6, and, in the case where m is 1, R.sub.1 is hydroxyl, C.sub.1 -C.sub.30 alkoxy, C.sub.3 -C.sub.30 alkoxy which is interrupted by oxygen, sulfur or >N--R.sub.13 ; C.sub.7 -C.sub.9 phenylalkoxy, C.sub.5 -C.sub.12 cycloalkoxy, C.sub.2 -C.sub.18 alkenyloxy, unsubstituted or C.sub.1 -C.sub.12 alkyl-substituted phenoxy, ##STR4## R.sub.16, r and M are as defined above, R.sub.19 and R.sub.20, independently of one another, are C.sub.1 -C.sub.4 alkyl, p is 1 or 2, and R.sub.6 is hydrogen or a radical of the formula (3), ##STR5## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.8 R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are as defined above, are described as stabilizers for organic materials against thermal, oxidative or light-induced degradation.

190. 发明授权

US5338730A Use of the (R) isomer of 2-[(2-octa-decyloxymethyl-tetrahydro-2-furanylmethoxy)-hydroxyphosphinyl oxy]-N,N,N-trimethylethanaminium hydroxide inner salt-4-oxide in treating multiple sclerosis 失效
标题翻译： 2 - [（2-八氢 - 癸氧基甲基 - 四氢-2-呋喃基甲氧基） - 羟基氧膦基氧基] -N，N，N-三甲基乙基氢氧化铵内盐-4-氧化物的（R）异构体在治疗多发性硬化
公开(公告)号：US5338730A
公开(公告)日：1994-08-16
申请号：US073215
申请日：1993-06-04
申请人： Heinrich Estermann , Prasad K. Kapa , Russell L. Underwood , William J. Houlihan
发明人： Heinrich Estermann , Prasad K. Kapa , Russell L. Underwood , William J. Houlihan
IPC分类号： C07D307/12 , C07F9/655 , C07F9/6574 , A61K31/665 , C07F9/141
CPC分类号： C07D307/12 , C07F9/65515 , C07F9/65742 , Y10S514/903
摘要： A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.
摘要翻译：制备2,2-双（羟基甲基） - 四氢呋喃单丁酸酯的（R）立体异构体的方法，包括使2,2-双（羟甲基） - 四氢呋喃的二酯进行酶水解。本发明还涉及通过本方法制备的新型（R）立体异构体及其更稳定的形式。此外，本发明涉及（R）立体异构体在制备药理活性化合物和由此制备的某些特定立体异构体的立体异构体中的用途。

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